Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 5.1.1.4 extracted from

  • Berneman, A.; Montout, L.; Goyard, S.; Chamond, N.; Cosson, A.; dArchivio, S.; Gouault, N.; Uriac, P.; Blondel, A.; Minoprio, P.
    Combined approaches for drug design points the way to novel proline racemase inhibitor candidates to fight Chagas disease (2013), PLoS ONE, 8, e60955.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.1.1.4

Cloned(Commentary)

Cloned (Comment) Organism
recombinant expression of His-tagged enzyme in Escherichia coli strain BL21(DE3) Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(E)-4-oxopent-2-enoic acid an irreversible strong competitive inhibitor, which hampers Trypanosoma cruzi intracellular differentiation and fate in mammalian host cells Trypanosoma cruzi
(E)-5-bromo-4-oxopent-2-enoic acid an irreversible strong competitive inhibitor, which hampers Trypanosoma cruzi intracellular differentiation and fate in mammalian host cells Trypanosoma cruzi
2-pyrrolecarboxylic acid
-
 Trypanosoma cruzi
4-bromopyrazole-3-carboxylic acid
-
 Trypanosoma cruzi
4-chloro-5-methyl-pyrazole-3-carboxylic acid
-
 Trypanosoma cruzi
4-chloropyrazole-3-carboxylic acid
-
 Trypanosoma cruzi
4-ethylpyrazole-3-carboxylic acid
-
 Trypanosoma cruzi
additional information synthesized soluble pyrazole derivatives prove to be weak or inactive TcPRAC inhibitors Trypanosoma cruzi
pyrazole-3-carboxylic acid
-
 Trypanosoma cruzi

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-proline Trypanosoma cruzi
-
 D-proline
-
 r

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-proline
-
 Trypanosoma cruzi D-proline
-
 r

Synonyms

Synonyms Comment Organism
PRAC
-
 Trypanosoma cruzi

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Trypanosoma cruzi

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
 assay at Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.006 0.01 2-pyrrolecarboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi
0.3
-
 4-chloropyrazole-3-carboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi
1
-
 4-bromopyrazole-3-carboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi
2
-
 pyrazole-3-carboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi
2
-
 4-ethylpyrazole-3-carboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi
2
-
 4-chloro-5-methyl-pyrazole-3-carboxylic acid recombinant His-tagged enzyme, pH 6.0, 37°C Trypanosoma cruzi